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| 1mg | ||
| 5mg | ||
| Other Sizes |
| ln Vitro |
In CHO-S cells overexpressing human OX40 (CHO-S-hOX40), cudarolimab (0.01, 1, 100, or 10,000 nM) binds to OX40 and partially inhibits OX40's binding to its ligand OX40L. With an EC50 of 4.432 nM, cudarolimab triggered the OX40-dependent NF-κB reporter in Jurkat-OX40 reporter cells co-cultured with Raji cells [1]. In a dose-dependent manner, cudarolimab (0.01, 0.1, 1, 10, 100, or 1000 nM) binds to activated CD4+ T cells in humans and active CD4+ T cells in cynomolgus monkeys [1]. In human CD4+ T cells, cudarolimab (0.4, 4.0, and 40.4 nM) enhances IL-2 secretion [1].
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| ln Vivo |
In human NOG mice with LoVo tumors, cudarolimab (10 mg/kg; i.p.; single dosage on days 3, 7, 11, 14, and 15) significantly decreased tumor volume[1]. In MC38 tumor-bearing OX40 knock-in mice, cudarolimab (0.1, 1, and 10 mg/kg; i.p.; single dose on days 6, 9, 12, and 16) markedly decreased tumor volume and increased tumor and spleen development. IFN-γ+ and IFN-α+ expression in CD8+ T cells[1]. Cudarolimab (i.p.; single dosage on days 10 and 14) at doses of 0.1, 1, and 10 mg/kg significantly decreased the expression of CD3+CD8+, CD3+CD4+, and CD4 in the tumors and spleens of OX40 knock-in mice having MC38 tumors with +CD25highFoxP3+ expression[1]. Cudarolimab's pharmacokinetic (PK) characteristics in cynomolgus monkeys[1] include: dose (mg/kg), Cmax (µg/mL), Tmax (h), AUC0-∞ (h·µg/mL), T1/2 (h), Cl (mL/h/kg), MRTlast (h) 0.1 3.07±0.40 0.08±0.00 347.98±99.30 162.98±103.01 0.31±0.08 186.34±110.68 0.5 9.78±3.27 0.40±0.78 1429.19± 607.21 129.47±114.44 0.40±0.14 63.10±15.29 0.27±0.09 212.29±114.61 12.5 296.57±58.05 0.40±0.78 33511.65±1498 2.36 120.30±153.26 0.44±0.20 114.93±87.66
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| Animal Protocol |
Animal/Disease Models: Humanized NOG mice bearing LoVo tumors[1].
Doses: 10 mg/kg. Route of Administration: intraperitoneal (ip) injection; single dose on days 3, 7, 11, 14 and 15. Experimental Results: decreased tumor volume. Animal/Disease Models: Human OX40 knock-in mice bearing MC38 tumors[1]. Doses: 0.1, 1 and 10 mg/kg. Route of Administration: intraperitoneal (ip) injection; single dose on days 6, 9, 10, 12, 14 and 16. Experimental Results: demonstrated anti-tumor activity. |
| References |
[1]. Kuang Z, et al. Development and characterization of a novel anti-OX40 antibody for potent immune activation. Cancer Immunol Immunother. 2020 Jun;69(6):939-950.
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| CAS # |
2244739-29-3
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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